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Synthesis and Pharmacological Evaluation of 4-Iminothiazolidinones for Inhibition of PI3 Kinase.
- Source :
-
Australian journal of chemistry [Aust J Chem] 2012 Jan 10; Vol. 65 (10), pp. 1396-1404. - Publication Year :
- 2012
-
Abstract
- The thiazolidinedione, compound 1 , has previously shown pan-inhibition of the phosphoinositide 3-kinase (PI3K) class I isoforms. We hypothesized the derivatization of the thiazolidinedione core of compound 1 could introduce isoform selectivity. We report the synthesis, characterization, and inhibitory activity of a novel series of 4-iminothiazolidin-2-ones for inhibition of the class I PI3K isoforms. Their synthesis was successfully achieved by multiple pathways described in this paper. Initial in vitro data of 28 analogues demonstrated poor inhibition of all class I PI3K isoforms. However, we identified an alternate target, the phosphodiesterases, and present preliminary screening results showing improved inhibitory activity.
Details
- Language :
- English
- ISSN :
- 0004-9425
- Volume :
- 65
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Australian journal of chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23997244
- Full Text :
- https://doi.org/10.1071/CH12140